A dopamine D1 receptor agonist
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A-77636 (hydrochloride)

Item No. 24316

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(1R,3S)-1-(aminomethyl)-3,4-dihydro-3-tricyclo[3.3.1.13,7]dec-1-yl-1H-2-benzopyran-5,6-diol, monohydrochloride
CAS Number
145307-34-2
Molecular Formula
C20H27NO3 • HCl
Formula Weight
365.9
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 33 mg/mlDMSO: 33 mg/mlEthanol: 33 mg/mlEthanol:PBS (pH 7.2) (1:6): 0.14 mg/ml
SMILES
OC1=CC=C2C(C[C@@H](C3(C[C@H](C4)C5)C[C@H]5C[C@H]4C3)O[C@H]2CN)=C1O.Cl
InChi Code
InChI=1S/C20H27NO3.ClH/c21-10-17-14-1-2-16(22)19(23)15(14)6-18(24-17)20-7-11-3-12(8-20)5-13(4-11)9-20;/h1-2,11-13,17-18,22-23H,3-10,21H2;1H/t11-,12+,13-,17-,18-,20?;/m0./s1
InChi Key
BWHPNJVKFAPVOG-WUAVIEMVSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $178

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    10 mg

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    Product Description

    A-77636 is a dopamine D1 receptor agonist (Ki = 40 nM).1 It induces activity equal to or greater than dopamine (Item No. 21992) in an adenylate cyclase assay of D1 receptor activity in fish retina and rat caudate putamen (EC50s = 7.4 and 1.1 nM, respectively) but does not show agonist activity at D2 receptors expressed in MMQ cells when used at concentrations up to 10 μM. A-77636 (10 μM) induces desensitization of dopamine-stimulated cAMP accumulation and downregulation of D1 receptors, reducing D1 receptor expression by 79% in C-6 glioma cells expressing monkey D1A receptors.2 In a marmoset model of Parkinson's disease induced by MPTP, A-77636 (3 μmol/kg, s.c.) increases locomotor activity 5.3-fold and reduces disease severity.1 Subcutaneous administration of A-77636 elicits cortical acetylcholine release at a dose of 1 μmol/kg.3 It also elicits over a 230% increase in cortical and hippocampal acetylcholine release when administered at a dose of 4 μmol/kg, an effect that is blocked by the D1 antagonist SCH 23390 (Item No. 15631).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kebabian, J.W., Britton, D.R., DeNinno, M.P., et al. A-77636: A potent and selective dopamine D1 receptor agonist with antiparkinsonian activity in marmosets. Eur. J. Pharmacol. 229(2-3), 203-209 (1992).

    2. Lewis, M.M., Watts, V.J., Lawler, C.P., et al. Homologous desensitization of the D1A dopamine receptor: Efficacy in causing desensitization dissociates from both receptor occupancy and functional potency. J. Pharmacol. Exp. Ther. 286(1), 345-353 (1998).

    3. Acquas, E., Day, J.C., and Fibiger, H.C. The potent and selective dopamine D1 receptor agonist A-77636 increases cortical and hippocampal acetylcholine release in the rat. Eur. J. Pharmacol. 260(1), 85-87 (1994).